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SB590885 是一种 B-Raf 抑制剂,Ki 值为 0.16 nM,对其选择性是对 c-Raf 的 11 倍多。
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SB590885 是一种 B-Raf 抑制剂,Ki 值为 0.16 nM,对其选择性是对 c-Raf 的 11 倍多。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 267 | 现货 | |
5 mg | ¥ 622 | 现货 | |
10 mg | ¥ 973 | 现货 | |
25 mg | ¥ 1,930 | 现货 | |
50 mg | ¥ 3,750 | 现货 | |
100 mg | ¥ 5,390 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,080 | 现货 |
产品描述 | SB590885 is an effective B-Raf inhibitor (Ki: 0.16 nM, in a cell-free assay). The selectivity of SB590885 for B-Raf is 11-fold greater over c-Raf, no acts to other human kinases. |
靶点活性 | B-Raf:0.16 nM(Ki) |
体外活性 | 在负荷突变体B-Raf表达的A375P黑色素瘤移植的小鼠体内,SB590885可使肿瘤发生率明显降低,且对肿瘤生长有一定抑制作用. |
体内活性 | 在表达致癌B-RafV600E的Colo205,HT29,A375P,SKMEL28,和MALME-3M细胞中,SB590885可有效抑制ERK磷酸化(EC50:28/58/290/58/190 nM),并抑制增殖(EC50:0.1/0.87/0.37/0.12/0.15 μM)。相比于c-Raf(Ki:1.72 nM),SB590885对B-Raf的选择性明显更高(Ki:0.16 nM)。与多激酶抑制剂BAY43-9006不同,SB590885稳定致癌B-Raf激酶域的活性结构。且对B-Raf亲和力很高(Kd:0.3 nM)。大多数具有BRAF V600E突变体而无CDK4突变体(451Lu,WM983和WM35)的黑色素瘤细胞系对SB590885十分敏感(IC50 <1 μM)。 |
细胞实验 | Cells are treated with increasing concentrations of SB590885 and incubated for 72 hours. Viable cells are quantified using CellTiter-Glo reagent and luminescence detection on a Victor 2V plate reader. Cells are prepared for cell cycle analysis on a Becton Dickinson FACScan. Data is acquired and analyzed using CellQuest v3.3 software.(Only for Reference) |
分子量 | 453.54 |
分子式 | C27H27N5O2 |
CAS No. | 405554-55-4 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | DMSO: 12.5 mg/mL (27.56 mM) | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
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